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Target
Glucagon receptor
Ligand
BDBM50110055
Substrate
n/a
Meas. Tech.
ChEMBL_72875 (CHEMBL684126)
IC50
23±n/a nM
Citation
Madsen, P; Ling, A; Plewe, M; Sams, CK; Knudsen, LB; Sidelmann, UG; Ynddal, L; Brand, CL; Andersen, B; Murphy, D; Teng, M; Truesdale, L; Kiel, D; May, J; Kuki, A; Shi, S; Johnson, MD; Teston, KA; Feng, J; Lakis, J; Anderes, K; Gregor, V; Lau, J Optimization of alkylidene hydrazide based human glucagon receptor antagonists. Discovery of the highly potent and orally available 3-cyano-4-hydroxybenzoic acid [1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide. J Med Chem 45:5755-75 (2002) [PubMed] Article
More Info.:
Target
Name:
Glucagon receptor
Synonyms:
GCGR | GL-R | GLR_HUMAN | Glucagon Receptor (GCGR) | Glucagon receptor (GlucR)
Type:
Enzyme
Mol. Mass.:
54026.92
Organism:
Homo sapiens (Human)
Description:
P47871
Residue:
477
Sequence:
MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
Inhibitor
Name:
BDBM50110055
Synonyms:
3-Chloro-4-hydroxy-benzoic acid [1-(4-isopropyl-benzyl)-1H-indol-4-ylmethylene]-hydrazide | 3-Chloro-4-hydroxy-benzoic acid [1-[1-(4-isopropyl-benzyl)-1H-indol-4-yl]-meth-(E)-ylidene]-hydrazide | CHEMBL153038 | N'-((1-(4-isopropylbenzyl)-1H-indol-4-yl)methylene)-3-chloro-4-hydroxybenzohydrazide
Type:
Small organic molecule
Emp. Form.:
C26H24ClN3O2
Mol. Mass.:
445.941
SMILES:
CC(C)c1ccc(Cn2ccc3c(\C=N\NC(=O)c4ccc(O)c(Cl)c4)cccc23)cc1